Synthesis and Anticancer Activities of Derivatives Chrysin Derivatives

Objective To synthetize a variety of chrysin derivatives and identify their antitumor activity in vitro. Methods Chrysin was applied as main raw materials and the 5-Bromosalicylic acid ester was added to the reaction system to synthesize chrysin derivatives in the etherification reaction. Then the MTT method was used to detect the anticancer activities of chrysin derivatives on human gastric cell line MGC-803 and human hepatocellular carcimoma cell Hep G2. Results The 50% inhibiting concentrations of compounds 2a, 2b and 4a on Hep G2 cells were lower than that of chrysin in vitro. Meanwhile, the 50% inhibiting concentrations of compounds 2a and 4a on Hep G2 cells were lower than that of positive control component 5-FU. The 50% inhibiting concentration of compound 3a on MGC-803 cells were also lower than that of chaysin and 5-FU. Conclusions The chemical structures of these compounds were confirmed by 1H NMR, MS method. The antitumor activity of compound 2a against Hep G2 cell and compound 3a against MGC-803 cell were better than 5-fluorouracil.